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首页> 外文期刊>Archiv der Pharmazie >Synthesis and antimicrobial evaluation of new pyrano4,3-bpyran and pyrano3,2-cchromene derivatives bearing a 2-thiophenoxyquinoline nucleus
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Synthesis and antimicrobial evaluation of new pyrano4,3-bpyran and pyrano3,2-cchromene derivatives bearing a 2-thiophenoxyquinoline nucleus

机译:带有2-噻吩氧基喹啉核的新型吡喃并4,3-b吡喃和吡喃并3,2-c色烯衍生物的合成和抗菌评价

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A new series of pyrano4,3-bpyran 4a-i and pyrano3,2-cchromene 6a-r derivatives bearing a 2-thiophenoxyquinoline nucleus were synthesized by reaction of 2-(4-(un)-substituted thiophenoxy)quinoline-3-carbaldehydes 2a-i with 6-methyl-4-hydroxypyran-2-one 3 and 4-hydroxy-6-(un)-substituted-2H- chromen-2-one 5a-b respectively and malononitrile at room temperature in the presence of KOH as a basic catalyst. All the compounds were screened against three Gram-positive bacteria (Streptococcus pneumoniae, Bacillus subtilis, Clostridium tetani), three Gram-negative bacteria (Salmonella typhi, Escherichia coli, Vibrio cholerae) and two fungi (Candida albicans, Aspergillus fumigatus) using the broth microdilution MIC (minimum inhibitory concentration) method. Upon antimicrobial screening, it was observed that the majority of the compounds were found to be active against Bacillus subtilis, Clostridium tetani and Candida albicans as compared to standard drugs. A new series of pyrano4,3-bpyran 4a-i and pyrano3,2-cchromene 6a-r derivatives bearing a 2-thiophenoxyquinoline nucleus were synthesized. All compounds were screened against three Gram-positive bacteria, three Gram-negative bacteria and two fungi. The majority of the compounds were found to be active against Bacillus subtilis, Clostridium tetani and Candida albicans as compared to standard drugs.
机译:以KOH为碱性催化剂,以2-(4-(un)-取代噻吩氧基)喹啉-3-甲醛2a-i与6-甲基-4-羟基吡喃-2-酮3和4-羟基-6-(un)-取代-2H-苯并吡喃-2-酮5a-b和丙二腈反应,合成了带有2-噻吩氧基喹啉核的吡喃并[4,3-b]吡喃4a-i和吡喃[3,2-c]色烯-2-酮5a-r衍生物。采用肉汤微量稀释MIC(最小抑制浓度)法对3种革兰氏阳性菌(肺炎链球菌、枯草芽孢杆菌、破伤风梭菌)、3种革兰氏阴性菌(伤寒沙门氏菌、大肠杆菌、霍乱弧菌)和2种真菌(白色念珠菌、烟曲霉)进行筛选。经抗菌药物筛选,发现与标准药物相比,大多数化合物对枯草芽孢杆菌、破伤风梭菌和白色念珠菌具有活性。合成了带有2-噻吩氧基喹啉核的新型吡喃并[4,3-b]吡喃4a-i和吡喃并[3,2-c]色烯6a-r衍生物。对3种革兰氏阳性菌、3种革兰氏阴性菌和2种真菌进行筛选。与标准药物相比,大多数化合物被发现对枯草芽孢杆菌、破伤风梭菌和白色念珠菌具有活性。

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